CAS No. : 9062-57-1
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|Cat. No. :||CS-7813|
|CAS No. :||9062-57-1|
|M. Wt. :|
|Solubility:||10 mM in DMSO|
Pentosan polysulfate is a potent and selective HIV inhibitor. IC50 & Target: HIV, NF-κB, TNF-alpha In Vitro: Pentosan polysulfate inhibits HIV-1 activity with an ED50 of 0.19 μg/mL in MT-4 cells. It inhibits HIV-1 antigen expression in HUT-78 cells at an ED50 of 0.02 μg/mL, and complete inhibition of HIV-1 antigen expression is obtained at a concentration of 4.0 μg/mL. No toxicity for MT-4 cells is observed with pentosan polysulfate at a concentration of 2500 μg/mL. The anticoagulant activity of pentosan polysulfate is more than ten-fold lower than that of heparin (14.4 and 177 U/mg, respectively). Pentosan polysulfate achieves its anti-HIV-1 activity at a concentration that is 370-fold below its anticoagulant threshold (1 U). Pentosan polysulfate inhibits virus adsorption to the cells, as is demonstrated by monitoring the association of radiolabeled HIV-1 virions with MT-4 cells. In Vivo: Pentosan polysulfate has been shown to decreases interstitial inflammation and glomerulosclerosis in 5/6 nephrectomized rats. Pentosan polysulfate treatment preserves renal function, significantly reduces albuminuria, and markedly decreases the severity of renal lesions, including tubulointerstitial inflammation. Pentosan polysulfate also reduces upregulation of TNFα and proinflammatory genes in aging diabetic kidneys.
Protocol:Cell Assay: MT-4 and HUT-78 cells are cultured in microtray wells in the presence of pentosan polysulfate (0-2500 μg/mL) added immediately after infection with 100 CCIDs0 of HIV-1 (CCIDs0 being the 50% cell culture infective dose). After 5 days incubation at 37°C, the number of viable ceils is determined by the 3'-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) method. Animal Administration: Mice with stable hyperglycemia at 18 months of age are selected for the study. Eighteen-month-old diabetic mice are randomly divided into pentosan polysulfate-treated (25 mg/kg/day in the drinking water) and control groups. Diabetic mice are followed for 4 months without insulin treatment. Mouse is housed individually and water intake is recorded every other day. Body weight and blood glucose levels are monitored weekly. Additionally, urine ketones are examined. Urine albumin excretion is measured bi-weekly.
Baba M, et al. Pentosan polysulfate, a sulfated oligosaccharide, is a potent and selective anti-HIV agent in vitro. Antiviral Res. 1988 Sep;9(6):335-43.
Wu J, et al. Inhibition of inflammation by pentosan polysulfate impedes the development and progression of severe diabetic nephropathy in aging C57B6 mice. Lab Invest. 2011 Oct;91(10):1459-71.
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